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ea0041ep774 | Nuclear receptors and Signal transduction | ECE2016

Optical isomers of statins enantiospecifically activate pregnane X receptor PXR and induce CYP2A6, CYP2B6 and CYP3A4 in human hepatocytes

Stepankova Martina , Dvorak Zdenek

Statins are drugs used for the treatment of hypercholesterolemia. Statins have two chiral centers in their molecules, thus they form four enantiomers (3R5R-, 3R5S-, 3S5R- and 3S5S-). Regarding the most frequently prescribed statins, following enantiopure formulations are used in the clinics: 3R5R-atorvastatin, 3R5S-rosuvastatin and 3R5S-fluvastatin. Individual enantiomers of one drug can qualitatively and quantitatively differ in their biological activities. In some cases, onl...